SAR study of 4-arylazo-3,5-diamino-1-pyrazoles: identification of small molecules that induce dispersal of biofilms

By screening of a collection of 50 000 small-molecule compounds, we recently identified 4-arylazo-3,5-diamino-1 H -pyrazoles as a novel group of anti-biofilm agents. Here, we report a SAR study based on 60 analogues by examining ways in which the pharmacophore can be further optimized, for example,...

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Published inRSC medicinal chemistry Vol. 12; no. 11; pp. 1868 - 1878
Main Authors Jansen, Charlotte U, Uhd, Jesper, Andersen, Jens B, Hultqvist, Louise D, Jakobsen, Tim H, Nilsson, Martin, Nielsen, Thomas E, Givskov, Michael, Tolker-Nielsen, Tim, Qvortrup, Katrine M
Format Journal Article
Published 17.11.2021
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Summary:By screening of a collection of 50 000 small-molecule compounds, we recently identified 4-arylazo-3,5-diamino-1 H -pyrazoles as a novel group of anti-biofilm agents. Here, we report a SAR study based on 60 analogues by examining ways in which the pharmacophore can be further optimized, for example, via substitutions in the aryl ring. The SAR study revealed the very potent anti-biofilm compound 4-(2-(2-fluorophenyl)hydrazineylidene)-5-imino-4,5-dihydro-1 H -pyrazol-3-amine ( 2 ). By screening of a collection of 50 000 small-molecule compounds, we recently identified 4-arylazo-3,5-diamino-1 H -pyrazoles as a novel group of anti-biofilm agents.
Bibliography:10.1039/d1md00275a
Electronic supplementary information (ESI) available: General methodologies; experimental and analytical Data. See DOI
ISSN:2632-8682
DOI:10.1039/d1md00275a